HPLC/MS研究国产盐酸班布特罗片及其代谢物特布他林人体生物等效性

目的研究国产班布特罗片剂和进口片剂进行人体生物等效性研究。方法20名健康受试者随机交叉给药,用液相色谱/质谱联用测定血浆中班布特罗其代谢物特布他林的浓度。结果经数据处理,单次口服国产和进口班布特罗片剂后班布特罗的药代动力学参数:AUC_0-t分别为(52±21)μg·h·L^-1和(51±20)μg·h·L^-1,T_max分别为(2.9±0.9)h和(2.6±0.7)h,C_max分别为(6.0±2.6)μg·L^-1和(6.2±2.9)μg·L^-1。特布他林:AUC_0-t分别为(191±30)μg·h·L^-1和(197±37)μg·h·L^-1,T_max分别为(4.2±1.0)h和(4.2±1.0)h,C_max分别为(10±5)μg·L^-1和(10±4)μg·L^-1。国产班布特罗片剂单次给药后的相对生物利用度为102%±8%(班布特罗),100%±12%(特布他林)。结论经统计学证明两制剂有生物等效性。

BIOEQUIVALENCE OF BAMBUTERAL AND ITS METABOLITES TERBUTALINE AFTER ORAL BAMBUTERAL TABLET IN HEALTHY VOLUNTEERS BY HPLC/MS

AIM: To study bioequivalence of bambuteral and its metablites terbutaline in 20 healthy male volunteers. METHODS: A single oral dose of domestic or imported bambuteral tablet was given according to a randomized 2-way cross-over design. The plasma bambuteral and terbutaline concentrations were determined by HPLC/MS. RESULTS: The pharmacokinetic parameters of domestic and imported bambuteral: AUC0-t were (52 +/- 21) microgram.h.L-1 and (51 +/- 20) microgram.h.L-1, Tmax were (2.9 +/- 0.9) h and (2.6 +/- 0.7) h, Cmax were (6.0 +/- 2.6) microgram.L-1 and (6.2 +/- 2.9) microgram.L-1, T1/2Ke were (11.2 +/- 2.3) h and (11.2 +/- 1.9) h, respectively; terbutaline: AUC0-t were (191 +/- 30) microgram.h.L-1 and (197 +/- 37) microgram.h.L-1; Tmax were (4.2 +/- 1.0) h and (4.2 +/- 1.0) h; Cmax were (10 +/- 5) microgram.L-1 and (10 +/- 4) microgram.L-1; T1/2Ke were (20 +/- 3) h and (21 +/- 4) h, respectively. The bioavaiability of the domestics was 102% +/- 8% (bambuteral) and 100% +/- 12% (terbutaline). CONCLUSION: The results demonstrate that the two forms of bambuteral and terbutaline were bioequivalent by analysis of variance, two-one sided test and 90% confidential limit.